Table 2.
IC50 values of Chembridge hit compounds against MtbTopI, human topoisomerase I (hTOPI) and E. coli DNA gyrase.
| Compound Number | Chembridge ID | MtbTopI Relaxation Inhibition (IC 50 , µM) | hTOPI Relaxation Inhibition (IC 50 , µM) | E. coli DNA Gyrase Supercoiling Inhibition (IC 50 , µM) |
|---|---|---|---|---|
| 7 | 49981944 | 2 | >500 | >500 |
| 8 | 9302190 | 62.5 | >500 | >500 |
| 9 | 37097280 | 62.5 | >500 | >500 |
| 10 | 88421238 | 62.5 | >500 | >500 |
| 11 | 73600812 | 62.5 | 250 | >500 |
| 12 | 80760557 | 62.5 | >500 | >500 |
| 13 | 17951480 | 62.5–125 | >500 | n.d. |
| 14 | 15044152 | 62.5–125 | n.d. | n.d. |
| 15 | 7931615 | 62.5–125 | n.d. | n.d. |
| 16 | 7875243 | 125 | n.d. | n.d. |
| 17 | 19138872 | 125 | n.d. | n.d. |
| 18 | 19046220 | 125 | n.d. | n.d. |
| 19 | 67687224 | 125 | n.d. | n.d. |
| 20 | 18538504 | 125 | n.d. | n.d. |
| 21 | 68171804 | 125 | n.d. | n.d. |
| 22 | 44982805 | 125 | n.d. | n.d. |
| 23 | 67941389 | 125 | n.d. | n.d. |
| 24 | 63920724 | 125 | n.d. | n.d. |
n.d. – not determined.